Crystalline Drug Aconitine-loaded Poly(d,l-Lactide-CoGlycolide) Nanoparticles: Preparation and in Vitro Release

Xuefan XU, Qingyu XIANG, Zhiyao HE, Yuehua LIU, Dan ZHOU, Xuan QIN, Tingting FAN, Zhirong ZHANG, Yuan HUANG
2010 Yakugaku zasshi  
This paper reports both the optimization of aconitine entrapment and its release from biodegradable poly(d,l-lactide-coglycolide) (PLGA) nanoparticles prepared using the O/W single-emulsion/solvent-evaporation technique. The in‰uence of several parameters, such as the initial aconitine mass, aqueous-phase pH, volume ratio of aqueous/organic phase (W/O), PLGA concentration in the organic phase, etc., on aconitine encapsulation were investigated. The optimized nanoparticles had an entrapment
more » ... an entrapment e‹ciency of 88.40±3.02% with drug loading capacity of 9.42±2.93%. Crystallization growth, which played a crucial role in hindering the incorporation of aconitine into the polymer carrier, was proposed. DiŠerential scanning calorimetry and X-ray powder diŠraction demonstrated that aconitine existed in an amorphous state or as a solid solution in the polymeric matrix. The in vitro release proˆles exhibited a sustained release of aconitine from nanoparticles and a pH-dependent character in phosphate-buŠered saline with diŠerent pH values. Moreover, aconitine-loaded PLGA nanoparticles could lead to improvement in the stability of aconitine. This work demonstrated the feasibility of encapsulating aconitine into PLGA nanoparticles using the O/W single-emulsion/solvent-evaporation technique.
doi:10.1248/yakushi.130.409 pmid:20190525 fatcat:6wcpt2layfalbpk6wcvzfrbdim